Pawar P K, Majumdar D K
Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences & Research, Formerly College of Pharmacy (University of Delhi), New Delhi, India.
Pharmazie. 2007 Nov;62(11):853-7.
The objective of present investigation was to study the in vitro permeation characteristics of moxifloxacin from oil drops through freshly excised goat, sheep, buffalo and rabbit corneas. Moxifloxacin, 0.043 to 0.048% (w/v) ophthalmic solutions with or without (0.5% v/v) benzyl alcohol were made in arachis, castor, cottonseed, olive, soybean, sunflower and sesame oils. Permeation studies were conducted by putting 1 ml oil formulation on cornea (0.50 cm2) fixed between donor and receptor compartments of an all glass modified Franz diffusion cell and measuring the drug permeated in receptor (containing 10 ml bicarbonate ringer, pH 7.4 at 37 degrees C under stirring) by spectrophotometry at 291 nm, after 120 min. Post permeation corneal hydration was measured to assess corneal damage. The study was designed with paired corneas i.e. one cornea of an animal received formulation without benzyl alcohol while the contralateral cornea received formulation with benzyl alcohol. Moxifloxacin ophthalmic solution in castor oil showed maximum permeation with all the corneas. Addition of benzyl alcohol, a preservative, to oil drops reduced permeation of moxifloxacin from each oil drop, with corneas of all the species. Partition experiments with moxifloxacin oil drops and phosphate buffer (pH 7.4) indicated higher partitioning of drug in the oil phase, in presence of benzyl alcohol. Thus results of permeation are consistent with the partition characteristics of drug between oil and aqueous phase. Corneal hydration obtained with all the formulations was between 75 to 80% indicating no corneal damage.
本研究的目的是研究莫西沙星从油滴中透过新鲜摘除的山羊、绵羊、水牛和兔角膜的体外渗透特性。在花生油、蓖麻油、棉籽油、橄榄油、大豆油、向日葵油和芝麻油中制备了含或不含（0.5% v/v）苯甲醇的0.043%至0.048%（w/v）莫西沙星滴眼液。通过将1 ml油制剂置于固定在全玻璃改良Franz扩散池供体和受体隔室之间的角膜（0.50 cm²）上进行渗透研究，并在搅拌下于37℃、pH 7.4的条件下，在受体（含10 ml碳酸氢盐林格液）中，120分钟后通过分光光度法在291 nm处测量透过的药物量。测量渗透后角膜的水合作用以评估角膜损伤。该研究采用配对角膜设计，即动物的一只角膜接受不含苯甲醇的制剂，而对侧角膜接受含苯甲醇的制剂。蓖麻油中的莫西沙星滴眼液在所有角膜上的渗透量最大。向油滴中添加防腐剂苯甲醇会降低莫西沙星从每种油滴中透过所有物种角膜的量。莫西沙星油滴与磷酸盐缓冲液（pH 7.4）的分配实验表明，在苯甲醇存在下，药物在油相中的分配更高。因此，渗透结果与药物在油相和水相之间的分配特性一致。所有制剂获得的角膜水合作用在75%至80%之间，表明没有角膜损伤。
